ENMD-1068 hydrochloride|CAS |DC Chemicals

Cas No.:
Chemical Name:	ENMD-1068 hydrochloride
Synonyms:	ENMD1068
SMILES:	O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN.Cl
Formula:	C₁₅H₂₉N₃O₂^.HCl
M.Wt:	319.87
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Cat. No.	Product name	Field of application
DC41699	FSLLRY-NH2	FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
DC40104	RWJ-56110 dihydrochloride	RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619. RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
DC73497	TFLLRN-NH2	TFLLRN-NH2 is a potent, PAR1-selective agonist peptide with EC50 of 1.9 uM.
DC73496	NRD-21	NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.
DC73495	1-Piperidine Propionic Acid	1-Piperidine Propionic Acid (1-PPA) is an allosteric Inhibitor of protease activated receptor-2 (PAR2) with IC50 of 2.3 uM.
DC71997	BMS-986141	BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.
DC70677	PAR2 antagonist C391	PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.C391 blocks both PAR2 Ca2+ and MAPK signalling pathways activated by peptidomimetics and/or proteinase activation.C391 effectively attenuated compound 48/80-induced thermal hyperalgesia in vivo.C391 blocked A. alternata-induced, PAR2-dependent Ca2+ and MAPK signalling in 16HBE14o- cells, as well as β-arrestin recruitment in HEK 293 cells.C391 effectively attenuated A. alternata-induced inflammation, mucus production, mucus cell hyperplasia and airway hyperresponsiveness in acute allergen-challenged murine models.
DC70501	I-287	I-287 is a potent, selective, orally active inhibitor of PAR2, negative PAR2 allosteric modulator, inhibits PAR2-mediated activation of Gq and G12/13 but not Gi/o proteins (IC50=45-390 nM); I-287 is a negative allosteric modulator (NAM) and not an orthosteric competitive antagonist of hPAR2. I-287 inhibits PAR2-mediated activation of DAG/Ca2+/PKC and RhoA/SRF-RE, as well as FAK and ERK1/2 signaling pathways, shows no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization. I-287 inhibits PAR2-induced secretion of IL-8 cytokine in vitro and reduces Freund's adjuvant (CFA)-induced paw edema model in mice.
DC70391	ENMD-1068 hydrochloride	ENMD-1068 is a novel selective PAR2 antagonist without inhibitory activity against thrombin-mediated PAR3 and PAR4 signaling; blocks TNFα production in synovial explants from patients with arthritis, and inhibits mast cell tryptase-induced recruitment of eosinophils into the pleural cavity of mice, dose dependently attenuates joint inflammation.